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Singulair

Singulair
Singulair is a leukotriene receptor antagonist that is used to prevent and treat asthma. It may also be prescribed for other conditions like runny nose allergies.

Brand: Montelukast

Availability: In Stock
Average Delivery Time: 9 Days
Exp. Date: May 2024
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Singulair 10 mg
360 pills - 10 mg
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$633.99 $1.76 $240.93 Add to cart
270 pills - 10 mg
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$485.25 $1.80 $170.94 Add to cart
180 pills - 10 mg
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$335.97 $1.87 $101.49 Add to cart
120 pills - 10 mg
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$233.95 $1.95 $57.69 Add to cart
90 pills - 10 mg
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$187.93 $2.09 $30.80 Add to cart
60 pills - 10 mg
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$132.91 $2.22 $12.91 Add to cart
30 pills - 10 mg $72.91 $2.43 No Add to cart
Singulair 5 mg
360 pills - 5 mg
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$424.99 $1.18 $162.89 Add to cart
270 pills - 5 mg
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$325.95 $1.21 $114.96 Add to cart
180 pills - 5 mg
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$224.99 $1.25 $68.95 Add to cart
120 pills - 5 mg
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$156.91 $1.31 $39.05 Add to cart
90 pills - 5 mg
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$125.91 $1.40 $21.06 Add to cart
60 pills - 5 mg $89.95 $1.50 $8.03 Add to cart
30 pills - 5 mg $48.99 $1.63 No Add to cart
Singulair 4 mg
360 pills - 4 mg
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$378.99 $1.05 $148.89 Add to cart
270 pills - 4 mg
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$295.11 $1.09 $100.80 Add to cart
180 pills - 4 mg
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$200.99 $1.12 $62.95 Add to cart
120 pills - 4 mg
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$137.97 $1.15 $37.99 Add to cart
90 pills - 4 mg
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$106.99 $1.19 $24.98 Add to cart
60 pills - 4 mg $74.93 $1.25 $13.05 Add to cart
30 pills - 4 mg $43.99 $1.47 No Add to cart

Product description

DRUG TITLE

Singulair (Montelukast)

Pharmacological action

Cysteinyl leukotrienes (LTC4, LTD4, LTE4) are strong inflammatory mediators - eicosanoids - that are released by a variety of cells, including mast cells and eosinophils. These important proasthmatic mediators bind to cysteinyl leukotriene receptors. Cysteinyl leukotriene type I receptors (CysLT1 receptors) are present in human airways (including bronchial smooth muscle cells, macrophages) and other proinflammatory cells (including eosinophils and some myeloid stem cells). Cysteinyl leukotrienes correlate with the pathophysiology of bronchial asthma and allergic rhinitis. In asthma, leukotriene-mediated effects include bronchospasm, increased mucus secretion, increased vascular permeability, and increased eosinophil counts. In allergic rhinitis, cysteinyl leukotrienes are released from proinflammatory cells of the nasal mucosa during the early and late phases of the allergic reaction after allergen exposure, which manifests as symptoms of allergic rhinitis. An intranasal test with cysteinyl leukotrienes demonstrated increased nasal airway resistance and symptoms of nasal obstruction.


Montelukast is a highly active oral medication that significantly improves inflammatory scores in bronchial asthma. According to biochemical and pharmacological analysis, montelukast binds with high affinity and selectivity to CysLT1 receptors without interacting with other pharmacologically important receptors in the airways (such as prostaglandin receptors, choline or β-adrenoreceptors). Montelukast inhibits the physiological action of cysteinyl leukotrienes LTC4, LTD4, LTE4 by binding to CysLT1 receptors without having a stimulatory effect on these receptors.


Montelukast inhibits CysLT receptors in the airways, as evidenced by its ability to block the development of bronchospasm in response to inhalation of LTD4 in patients with bronchial asthma. A dose of 5 mg is sufficient to stop LTD4-induced bronchospasm.


Montelukast induces bronchodilation within 2 h after oral administration and may supplement bronchodilation induced by beta2-adrenomimetics.


Pharmacokinetics

Absorption


After oral administration, montelukast is rapidly and almost completely absorbed. Cmax is reached in 2 hours in adults when chewable 5 mg tablets are taken on an empty stomach. The average bioavailability when taken orally is 73%. Food intake has no clinically significant effect during long-term use.


Distribution


Binding of montelukast to plasma proteins is more than 99%. Vd in equilibrium is on average 8-11 liters. Studies performed on rats with radioactively labeled montelukast indicate minimal penetration through the HEB. In addition, the concentration of labeled montelukast 24 h after administration was minimal in all other tissues.


Metabolism


Montelukast is actively metabolized. When used in therapeutic doses in adults and children, plasma concentrations of montelukast metabolites are undetectable in equilibrium.


In vitro studies using human liver microsomes have shown that cytochrome P450 system isoenzymes are involved in the metabolism of montelukast: CYP3A4, 2C8 and 2C9. According to the results of the studies, conducted in vitro on human liver microsomes, in therapeutic concentration in plasma Montelukast does not inhibit CYP3A4, 2C9, 1A2, 2A6, 2C19 and 2D6 isoenzymes.


Excretion


Plasma clearance of montelukast in healthy adults is on average 45 ml/min. After ingestion of radioactively labeled montelukast, 86% of it is excreted in the feces within 5 days and less than 0.2% in the urine, confirming that montelukast and its metabolites are excreted almost exclusively with the bile.


The T1/2 of montelukast in young healthy adults is 2.7 to 5.5 h. The pharmacokinetics of montelukast remain almost linear when administered orally at doses greater than 50 mg. When taking montelukast in the morning and evening hours no differences in pharmacokinetics are observed. When receiving montelukast at a dose of 10 mg once daily a moderate (about 14%) cumulation of the active substance in plasma is observed.


Pharmacokinetics in special clinical cases


The pharmacokinetics of montelukast in women and men are similar.


In a single oral administration of montelukast at a dose of 10 mg, the pharmacokinetic profile and bioavailability are similar in elderly and young patients. T1/2 of montelukast from plasma is slightly longer in the elderly. No dose adjustment is required in elderly patients.


No differences in clinically significant pharmacokinetic effects were found in patients of different races.


In patients with mild to moderate hepatic insufficiency and clinical manifestations of liver cirrhosis a delay in metabolism of montelukast was noted, accompanied by an increase in AUC by approximately 41% after a single dose of 10 mg. The excretion of montelukast is slightly increased in these patients compared to healthy subjects (mean T1/2 is 7.4 h). There is no need to change the dose of montelukast for patients with mild to moderate hepatic impairment. There are no data on the nature of the pharmacokinetics of montelukast in patients with severe hepatic impairment (more than 9 points on the Child-Pugh scale).


Because montelukast and its metabolites are not excreted with the urine, the pharmacokinetics of montelukast in patients with renal insufficiency has not been evaluated. No dose adjustment is required in this group of patients.

Contraindications to use

Hypersensitivity to any of the components of the drug;

Childhood under 2 years of age;

phenylketonuria.

Administration during pregnancy and lactation

Syngular should be used during pregnancy and lactation only if the expected benefits to the mother exceed the potential risk to the fetus or child.


According to the available published data from prospective and retrospective cohort studies of montelukast in women during pregnancy whose children were evaluated for severe congenital malformations, no risks associated with taking the drug have been identified. The available studies have methodological limitations, including small sample sizes, in some cases retrospective data collection, and unmatched comparison groups.


It is not known whether montelukast is excreted with breast milk. Since many drugs are excreted with the breast milk, it is necessary to take this into account when prescribing Singulair during breastfeeding.


Administration in liver dysfunction

For patients with mild or moderate hepatic impairment, no special dosage adjustment is required.


There are no data about the character of pharmacokinetics of montelukast in patients with severe hepatic impairment (more than 9 points by Child-Pugh scale).


Use in renal impairment

No special dosage adjustment is required for patients with renal insufficiency.


Administration in children

Contraindicated: Children under 2 years of age.


Administration in elderly patients

No special dosage adjustment is required for elderly patients.

Indications of the drug Singulair

  • prophylaxis and long-term treatment of bronchial asthma in children aged from 2 to 5 years, including prevention of daytime and nighttime symptoms, treatment of bronchial asthma in patients with hypersensitivity to acetylsalicylic acid and prevention of exercise-induced bronchospasm;
  • relief of daytime and nighttime symptoms of seasonal and/or year-round allergic rhinitis in children aged 2 to 5 years.


Dosage regimen

The drug is taken orally once a day regardless of meals. For the treatment of bronchial asthma, Singular® should be taken in the evening. In treatment of allergic rhinitis, the drug may be taken at any time of the day if desired by the patient. Patients with bronchial asthma and allergic rhinitis should take 1 tablet of Singular once daily in the evening.


Children of 2 to 5 years of age in case of bronchial asthma and/or allergic rhinitis are prescribed in dose of 4 mg (1 chewable tablet)/day.


General guidelines


The therapeutic effect of Singulair on the indices reflecting the course of bronchial asthma develops within the first day. The patient should continue taking Singulair both during the period of achieving control of bronchial asthma symptoms and during periods of exacerbation of bronchial asthma.


No special dose adjustment is required for elderly patients, patients with renal insufficiency and patients with mild or moderate hepatic impairment, as well as depending on sex.


Administration of Singulair concomitantly with other types of bronchial asthma treatment